Kinase Chemistry – Just a year and a half behind the times.

Archive for the ‘clinical’ Category

Asco Abstracts

Posted by kinasepro on May 15, 2009


Posted in clinical | Leave a Comment »

UCB’s got a chart

Posted by kinasepro on October 15, 2008

go check it out.

Posted in clinical, General Interest | Leave a Comment »


Posted by kinasepro on December 7, 2007

Targegen’s got a press release:

Plans to initiate a multi-center clinical trial of TG101348, an internally discovered, oral, potent, and highly selective JAK2 inhibitor in January, 2008

A poster at ASH:

…Dual-Acting JAK2/FLT3 Small Molecule Kinase Inhibitor for the Treatment of AML

and some pyrimidines in WO/2007/053452:


Posted in biotech, clinical, Flt3, JAK | Leave a Comment »


Posted by kinasepro on October 22, 2007

Abstracts are up, and B is the one you’ll be looking for.

News of the day:

In pts [patients] with PRC, XL-880 demonstrated antitumor activity

Name Target Company Phase
AZD-2171 Vegf c-Kit Pdgfr-β AstraZeneca ph2
AZD-2171 Vegf c-Kit Pdgfr-β AstraZeneca ph2
PD-325901 Mek Pfizer ph2
XL-647 ErbB1,2 Vegfr-2 Exelixis ph2
XL-880 c-Met Vegf Exelixis ph2
ARQ-197 c-Met Arqule ph1
BAY-579352 Vegfr-2,3 c-Kit Pdgfr-β Bayer ph1
BAY-734506 c-Kit Ret Pdgfr Raf Bayer ph1
BIBW-2992 ErbB (irrev) BI ph1
PD-325901 Mek Pfizer ph1
PF-299804 ErbB (irrev) Pfizer ph1
Ticribine Akt VioQuest ph1
XL-647 ErbB 1,2 Vegfr-2 Exelixis ph1
XL-820 Vegfr c-Kit Pdgfr Exelixis ph1
XL-880 c-Met Vegf Exelixis ph1
ARRY-543 ErbB1, 2 Array ph1
AT-13148 Akt Rock PKA Astex  
AV-951 Vegf Aveo ph1
BAY-734506 c-Kit Ret Pdgfr Raf Bayer  
BMS-698769 c-Met BMS  
CEP-11981 Tie2 Vegfr Cephalon  
CUDC-101 HDAC / ErbB Curis  
NVP-BEZ235 Pi3k Novartis  
OSI-906 IGF-1R Osi  
RDEA-119 Mek Ardea  
SGX-523 c-Met SGX  
SR-13654 Src SRI  
XL-765 Pi3k, mTOR Exelixis  
XL-820 c-Kit Exelixis  
XL-844 Chk1, 2 Exelixis  
ZD-6474 Vegfr-2 EGFR    
ZM 447439 Aurora    
CRT-59359 PKD CRT  

Duplicates and phase field just reflect the subject of the poster / reported trial, click for more details.

Posted in clinical | 1 Comment »

Steal This Document

Posted by kinasepro on October 10, 2007

You may have noticed the Ro5 tab above. Here’s the spreadsheet.

To the best of my knowledge it’s the most complete list of clinical stage kinase inhibitors in existence. There are bound to be errors and omissions though, so while I of course don’t want anything proprietary please send me references and structures as appropriate. I appreciate the help.

Posted in clinical, General Interest | 10 Comments »

Clinical Roundup

Posted by kinasepro on October 9, 2007

Pharmacopoeia – earned a milestone for p38 inhibitor BMS-582949 going ph2.

Incyte – reported on ph2 Jak inhibitor INCB-18424 (?WO/2005/105814, 2B7A) (decent webcast here The short of it: pretty much the same as steroids … no adverse effects at any dose. check in ~8 minutes).

Exelixis – will bundle reports for ph2 XL-880, XL-647, and ph1 XL-184, XL820, and XL-147 at AACR later this month. The Fools think GSK will pick up 880 and I tend to agree.

Ambit talked about a lot at UBS and updates on AC-220 (ph1 FLT3 inhibitor).

Ardea (RDEA)- is preparing to list on the Nasdaq and has RDEA-119 about to hit ph1.

SGX – spins a yarn suggesting that Novartis took a pass on SGX-393. IND for a different compound expected mid ’08. (Webcast on Thursday)

Ariad – knows all about T315I and SGX… Still no structure for AP-24534 though… IND expected end of the year.

S*Bio – has SB-1518 an oral Jak2 (V617F) inhibitor in development: WO/2007/058628, WO/2007/058627

Posted in clinical | 2 Comments »

clinical roundup

Posted by kinasepro on July 26, 2007

Supergen initiates dosing of flt3 inhibitor MP-470: ph1 ‘advanced-stage solid tumors.’

Entremed initiates trial for Aurora inihbitor MKC-1: Ph1 Leukemia

Kinex gets the FDA go-ahead for Src inhibitor KX2-391: lymphoma or solid tumors (though despite the press release, it’s not the first non-atp competitive kinase inhibitor to enter the clinic. The MEK inhibitors were)

Posted in clinical | Leave a Comment »


Posted by kinasepro on February 13, 2007

Rigel’s Aurora inhibitor R-763 going Ph1 for ‘Hematological Malignancies’. It’s in Ph1 for solid tumors already. hmm… I thought they had to call it ‘EMD Serono’ in USA.  Merck DE # is: AS703569

So it’s looking like: WO/2006/055561 and before that: WO/2005/118544


Neeto – looks like they resolve the enantiomers via:

Even neeter-0 they show a couple xenos

Posted in Aurora, clinical, Merck DE, Rigel | 2 Comments »


Posted by kinasepro on January 5, 2007

Making some bold claims, Innovive gets orphan status for INNO-406 / NS-187



Posted in bcr abl, clinical, lyn | 3 Comments »


Posted by kinasepro on December 20, 2006

Exelixis is on fire these days. 518’s IND is in the books.

Posted in clinical, Exelixis, MEK | Leave a Comment »